CSRM617 hydrochloride (E4312-GRP)

CSRM617 hydrochloride is a selective small-molecule inhibitor of the transcription factor ONECUT2 (OC2, a master regulator of androgen receptor) with a Kd of 7.43 uM in SPR assays, binding to OC2-HOX domain directly. It induces apoptosis by appearance of cleaved Caspase-3 and PARP and is well tolerated in the prostate cancer mouse model.